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The rise of antibiotic resistance is of great clinical concern. One approach to reducing the development of resistance is to co-administer two or more antibiotics with different modes of action. However, it can be difficult to control the distribution and pharmacokinetics of two drugs to ensure both concentrations remain within the range of therapeutic efficacy whilst avoiding adverse effects. Hybrid drugs, where two drugs are linked together with a flexible linker, have been explored, but the resultant large, flexible molecules can have poor bioavailability. We have developed a chimeric approach using click chemistry where the pharmacophores of two drugs are overlapped into a single smaller, more drug-like molecule. Design and selection of compounds were assisted by in silico structural docking. We prepared a series of compounds that include candidates showing activity against the targets of both trimethoprim; dihydrofolate reductase, and ciprofloxacin; DNA gyrase and topoisomerase IV. The resultant triazole containing molecules show modest, but broad spectrum activities against drug sensitive and resistant Gram-negative and Gram-positive bacteria, with no observable cytotoxicity.

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Reference£º
1,732-Naphthyridine – Wikipedia,
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A series of new C-7 substituted hydrazino quinolones and naphthyridines were prepared and tested for antibacterial activity. The hydrazine bridge at the C-7 position did not favor the antibacterial activity, whereas the nature of other substituents at N-1, C-5 and C-8 did noticeably influence the antibacterial activity. The 7-(1-aminomorpholino) derivatives exhibited superior antibacterial activity against Gram-positive and inferior activity against Gram-negative bacteria than the 7-(1-aminopiperazinyl) derivatives. Substitution of the quinolone at position-1 with cyclopropyl was the most beneficial for antibacterial activity among the series of compounds prepared.

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PRINCIPIA BIOPHARMA INC.; LOU, Yan; OWENS, Timothy, Duncan; BRAMELD, Kenneth, Albert; GOLDSTEIN, David, Michael

Provided herein are compounds, such as a compound of Formula (I), as described herein, or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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A series of novel fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results revealed that 19b2 shows good activity against MTB H37Rv ATCC 27294 (MIC: <0.25 I1/4g/mL) and MDR-MTB 6133 clinical isolate (MIC: 0.11 I1/4g/mL). Most of them have potent potency against Gram-positive strains, although they are generally poor active against Gram-negative strains. Especially, compounds 22b1 and 23a3 (MICs: <0.008-8 I1/4g/mL) were found to 2-128 times more potent than ciprofloxacin and levofloxacin against all of the tested Gram-positive strains including quinolone-resistant MRSA, MRSE, Enterococcus faecium and Enterococcus faecalis One of the oldest and most widely used commercial enzyme inhibitors is aspirin, category: naphthyridine, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 100361-18-0

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Eisai Co., Ltd.

The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2 represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; andB represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. COA of Formula: C12H8ClFN2O3, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 100361-18-0, name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid. In an article£¬Which mentioned a new discovery about 100361-18-0

HETERO DRUGS LIMITED

The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth- yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.

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Nanjing Gentai Pharmaceutical Co., Ltd.; Chen Rongyao; Shen Yu

The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, solvate, hydrate, active metabolite, polymorph, ester, isotopic compound, stereoisomer or prodrug, a pharmaceutical composition comprising a compound of formula I and its use as IDO inhibitor for the preparation of a medicament for preventing or treating cancer, viral infection, depression, cataract, organ transplantation rejection, or autoimmune disease thereof. (by machine translation)

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Henan University; Yan, Jiang; Wu, Shumin; Wang, Rui; Ni, Lili; Yang, Tong; Hu, Guojiang

The invention discloses a 1? Cyclopropyl? 7? Aminomethyl triazole? fluorine naphthyridine alkone carboxylic acid derivatives and its preparation method and application, the following chemical structural formula I: In formula I, R is dimethylamino, diethylamino, piperidinyl, morpholinyl, pyrrolidinyl, piperazinyl or substituted piperazinyl. A of the present invention 1? Cyclopropyl? 7? Aminomethyl triazole? fluorine naphthyridine alkone carboxylic acid derivatives, has been realized in the superiority pharmocology skeleton- cyclopropane fluorine naphthyridine alkone carboxylic acid and effective substituent 7? Amino is inserted between triazole heterocycle function, so as to improve the activity for resisting of the new compounds, can be used as new development of new antibacterial active substance of the anti-infection drugs structure. (by machine translation)

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100361-18-0, Name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid, belongs to naphthyridine compound, is a common compound. category: naphthyridineIn an article, once mentioned the new application about 100361-18-0.

WARNER-LAMBERT COMPANY LLC

Compounds of formula (I) wherein A is formula (II), formula (III) or formula (IV), and B is formula (V), formula (VI), or formula (VII), can be used in a variety of applications including use as antibacterial agents.

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The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3?-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.

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